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1. 发明专利

IL174252D0 BENZOXAZOLE ACETONITRILE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：IL174252D0
公开(公告)日：2006-08-01
申请号：IL17425206
申请日：2006-03-12
申请人： GAILLARD PASCALE , GOTTELAND JEAN PIERRE , MATTHIAS SCHWARZ , PAGE PATRICK , THOMAS RUSSEL J , SERONO LAB , APPLIED RESEARCH SYSTEMS
IPC分类号： A61K31/423 , A61P3/10 , C07D20100101 , C07D413/06 , C07D413/14 , C07D491/10
摘要： The present invention is related to benzoxazole acetonitriles as well as to pharmaceutical formulations containing such benzoxazole acetonitriles pof formula (I). Said benzoxazole acetonitriles are useful in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles (I). A is a pyrimidinyl.L is a secondary or tertiary amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom. selected from N, O, S or L is an acylamino moiety. R 1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, C 1 C 6 -alkYl, C 2 -C 6 -alkenYl, C 2 -C 6 -alkynyl or C 1 -C 6 -alkoxy, aryl, halogen, carboxy, aminocarbonyl, cyano or hydroxy.

3. 发明申请

WO2004071390A3 PIPERAZINE-2-CARBOXAMIDE DERIVATIVES 审中-公开
公开(公告)号：WO2004071390A3
公开(公告)日：2004-08-26
申请号：PCT/EP2004/050093
申请日：2004-02-06
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , PAGE, Patrick , JORAND-LEBRUN, Catherine , THOMAS, Russel J. , SCHWARZ, Matthias
发明人： PAGE, Patrick , JORAND-LEBRUN, Catherine , THOMAS, Russel J. , SCHWARZ, Matthias
IPC分类号： A61K31/495
摘要： The present invention is related to piperazine -2-carboxamide derivatives of formula (I) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. Wherein A, X, Y, R 1 and R 2 are as defined in the description.

4. 发明申请

WO2005011685A1 ARYL DICARBOXAMIDES 审中-公开
公开(公告)号：WO2005011685A1
公开(公告)日：2005-02-10
申请号：PCT/EP2004/051558
申请日：2004-07-20
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , THOMAS, Russel, J. , SWINNEN, Dominique , PONS, Jean-François , BOMBRUN, Agnès
发明人： THOMAS, Russel, J. , SWINNEN, Dominique , PONS, Jean-François , BOMBRUN, Agnès
IPC分类号： A61K31/426
CPC分类号： A61K31/16 , A61K31/166 , A61K31/167 , A61K31/426 , C07C237/42 , C07C255/57 , C07C2601/08 , C07C2601/14 , C07D277/30 , C07D277/56
摘要： The present invention is related to aryl dicarboxamides of formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycernia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholes-terolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of aryl dicarboxamides of formula (I) to modulate, notably to inhibit the activity of PTPs. A is an airninocarbonyl moiety; Cy is an aryl, heteroaryl, aryl-heteroaryl, heteroaryl-aryl, aryl-aryl, cycloalkyl or heterocycle group; n is either 0 or 1; R 1 and R 2 are independently from each other is selected from the group consisting of hydrogen or C 1 -C 6 -alkyl; R 4 and R 5 are each independently from each other selected from the group consisting of H, hydroxy, C 1 -C 6 alkyl, carboxy, C 1 -C 6 alkoxy, C 1 -C 3 alkyl carboxy, C 2 -C 3 alkenyl carboxy, C 2 -C 3 alkynyl carboxy, amino or R 4 and R 5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R 4 or R 5 is not a hydrogen or C 1 -C 6 alkyl.
摘要翻译：本发明涉及式（I）的芳基二甲酰胺和其用于治疗和/或预防由胰岛素抵抗或高血糖引起的肥胖和/或代谢障碍，其包括I型和/或II型糖，葡萄糖耐量不足，胰岛素抵抗，高脂血症，高甘油三酯血症，高胆固醇血症，多囊卵巢综合征（PCOS）。特别地，本发明涉及式（I）的芳基二羧酰胺的用途，特别是抑制PTP的活性。 A是空气羰基部分; Cy是芳基，杂芳基，芳基 - 杂芳基，杂芳基 - 芳基，芳基 - 芳基，环烷基或杂环基团; n为0或1; R 1和R 2彼此独立地选自氢或C 1 -C 6 - 烷基; R 4和R 5各自独立地选自H，羟基，C 1 -C 6烷基，羧基，C 1 -C 6烷氧基，C 1 -C 3烷基羧基，C 2 -C 3烯基羧基，C 2 -C 3炔基羧基，氨基或R 4和R 5可以形成不饱和或饱和的杂环，其中R 4或R 5中的至少一个不是氢或C 1 -C 6烷基。

5. 发明申请

WO2012076413A1 COMPOUND FOR THE TREATMENT OF TUMOURS AND TUMOUR METASTASES 审中-公开
标题翻译：用于治疗肿瘤和肿瘤细胞的化合物
公开(公告)号：WO2012076413A1
公开(公告)日：2012-06-14
申请号：PCT/EP2011/071630
申请日：2011-12-02
申请人： SIENA BIOTECH S.P.A. , PERICOT MOHR, Gal.la , THOMAS, Russel J. , MINETTO, Giacomo , BELLINI, Marta , WIEDENAU, Paul H. , BETTI, Matteo
发明人： PERICOT MOHR, Gal.la , THOMAS, Russel J. , MINETTO, Giacomo , BELLINI, Marta , WIEDENAU, Paul H. , BETTI, Matteo
IPC分类号： C07D213/38 , C07D213/26 , A61K31/4418 , A61P35/00 , A61P35/02 , A61P35/04
CPC分类号： C07D401/10 , C07C45/63 , C07D213/04 , C07D213/26
摘要： The invention relates to a Smoothened receptor ligand which antagonises the Hedgehog pathway, to pharmaceutical compositions and therapeutic applications thereof, processes for obtaining this compound and novel intermediates useful in these processes.
摘要翻译：本发明涉及拮抗Hedgehog途径的平滑受体配体，药物组合物及其治疗应用，获得该化合物的方法和用于这些方法的新型中间体。

6. 发明申请

WO2004071390A2 PIPERAZINE-2-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：哌嗪-2-羧酰胺衍生物
公开(公告)号：WO2004071390A2
公开(公告)日：2004-08-26
申请号：PCT/EP2004050093
申请日：2004-02-06
申请人： APPLIED RESEARCH SYSTEMS , PAGE PATRICK , JORAND-LEBRUN CATHERINE , THOMAS RUSSEL J , SCHWARZ MATTHIAS
发明人： PAGE PATRICK , JORAND-LEBRUN CATHERINE , THOMAS RUSSEL J , SCHWARZ MATTHIAS
IPC分类号： A61K6/00 , A61K31/16 , A61K31/495 , A61P15/06 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D521/00 , A61K
CPC分类号： C07D231/12 , A61K31/16 , A61K31/495 , C07D233/56 , C07D241/04 , C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： The present invention is related to piperazine -2-carboxamide derivatives of formula (I) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. Wherein A, X, Y, R and R are as defined in the description.
摘要翻译：本发明涉及式（I）的哌嗪-2-甲酰胺衍生物，其用于治疗和/或预防早产，早产，痛经和用于在剖宫产分娩前停止劳动。其中A，X，Y，R 1和R 2如说明书中所定义。

7. 发明申请

WO2003106455A1 AZOLE METHYLIDENE CYANIDE DERIVATIVES AND THEIR USE AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译：氨基甲基氰化物衍生物及其作为蛋白激酶调节剂的用途
公开(公告)号：WO2003106455A1
公开(公告)日：2003-12-24
申请号：PCT/EP2003/050225
申请日：2003-06-13
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , Gaillard, Pascale , Gotteland, Jean-Pierre , Jeanclaude-Etter, Isabelle , Schwarz, Matthias , Thomas, Russel, J.
发明人： Gaillard, Pascale , Gotteland, Jean-Pierre , Jeanclaude-Etter, Isabelle , Schwarz, Matthias , Thomas, Russel, J.
IPC分类号： C07D417/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D417/06 , C07D417/12 , C07D417/14 , C07D495/10
摘要： The present invention is related to azole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such azole derivatives. Said azole derivatives are modulators of the protein kinase signalling pathways, particularly the one involving c-Jun N-terminal kinase and/or Glycogen Kinase Synthase 3. The present invention is furthermore related to novel azole derivatives as well as to methods of their preparation. X is O, S or NR 0 , with R 0 being H or an unsubstituted or substituted C 1 -C 6 alkyl; A is 2-pyridyl, 3-pyridyl, 4-pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl or triazinyl group.
摘要翻译：本发明涉及特别用作药物活性化合物的唑衍生物以及含有这种唑衍生物的药物制剂。所述唑衍生物是蛋白激酶信号通路的调节剂，特别是涉及c-Jun N-末端激酶和/或糖原激酶合成酶3的调节剂。本发明还涉及新型唑衍生物及其制备方法。 X是O，S或NR 0，其中R 0是H或未取代或取代的C 1 -C 6烷基; A是2-吡啶基，3-吡啶基，4-吡啶基，哒嗪基，嘧啶基，吡嗪基或三嗪基。

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